Design, synthesis, and biological evaluation of 2-(4-(methylsulfonyl) phenyl) indole derivatives with promising COX-2 inhibitory activity

J App Pharm Sci. 2018; 8(11): 1-8

doi: 10.7324/JAPS.2018.81101

Ahmed M. M. Shaker, Eman K. A. Abdelall, Khaled R. A. Abdellatif, Hamdy M. Abdel-Rahman.

Abstract
A series of 2-(4-(methylsulfonyl)phenyl)-1-substituted-indole derivatives 4a-f was designed and synthesized as indomethacin analogs; All compounds were evaluated for their in vitro COX-2 inhibitory activity as well as in vivo anti-inflammatory activity using indomethacin as reference drug. All synthesized compounds showed good anti-inflammatory activity and more selectivity for COX-2 inhibition. Molecular modeling study is performed and the results were in agreement with that obtained from in vitro COX-2 inhibition assays. Key words: Indole; Indomethacin; Anti-inflammatory activity; selective COX-2; Molecular modeling.